| AID483790 | Clearance in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483800 | Terminal half life in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID657810 | Terminal half life in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID657844 | Plasma protein binding in po dosed mouse after 4 hrs | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID1151435 | Inhibition of adipose tissue-derived 11beta-HSD1 (unknown origin) assessed as concentration required for maximal inhibition | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID483802 | Inhibition of CYP3A4 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483804 | Inhibition of CYP1A2 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID657808 | Clearance in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483806 | Inhibition of CYP2C19 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483808 | Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 5 mg/kg, po measured at 4 hrs by ELISA | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483792 | Terminal half life in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID657826 | Ratio of drug level in adipose tissue fat to plasma of mouse at 50 mg/kg, po | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483807 | Metabolic stability in liver microsomes | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483788 | Terminal half life in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID657812 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID1151434 | Inhibition of adipose tissue-derived 11beta-HSD1 (unknown origin) | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID483787 | Volume of distribution at steady state in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID1071798 | Inhibition of 11beta-HSD1 in mouse liver microsomes using cortisone as substrate after 2 hrs by HTRF assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
| 3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitor. |
| AID657805 | Inhibition of human 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone as substrate by scintillation proximity assay | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483812 | Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 15 mg/kg, po measured at 8 hrs by ELISA | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID657815 | Half life in CD1 mouse at 2 mg/kg, iv and 10 mg/kg, po | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483821 | Antiobesity activity in diet-induced obese mouse assessed as decrease in body weight at 5 mg/kg administered QD via high fat-diet for 13 days measured after day 13 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID1218573 | Oral bioavailability in rat | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
| Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers. |
| AID657813 | Clearance in CD1 mouse at 2 mg/kg, iv and 10 mg/kg, po | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483803 | Inhibition of CYP2D6 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID1218574 | Volume of distribution at steady state in rat | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
| Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers. |
| AID483801 | Bioavailability in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483794 | Clearance in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483797 | Bioavailability in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483805 | Inhibition of CYP2C9 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483789 | Bioavailability in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483799 | Volume of distribution at steady state in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483795 | Volume of distribution at steady state in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID1218572 | Plasma protein binding in rat | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
| Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers. |
| AID657806 | Inhibition of human 11beta-HSD1 expressed in CHO cells | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID1218571 | Plasma protein binding in human | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
| Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers. |
| AID657843 | Free plasma concentration in po dosed mouse after 4 hrs | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483815 | Antidiabetic activity in diet-induced obese mouse assessed as decrease in plasma insulin level at 25 to 50 mg/kg, po administered via gavage BID for 13 days measured after day 13 by glucose tolerance test | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483818 | Antidiabetic activity in diet-induced obese mouse assessed as mild improvement of glucose tolerance at 25 to 50 mg/kg, ip BID for 13 days measured on day 14 after 12 hrs of fasting by glucose tolerance test | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483782 | Displacement of [3H]-cortisone human 17beta-HSD1 expressed in HEK293 cells after 30 mins by scintillation proximity assay | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID657816 | Oral bioavailability in CD1 mouse at 10 mg/kg | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483785 | Inhibition of glucocorticoid receptor | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483813 | Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 50 mg/kg, po measured at 8 hrs by ELISA | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483784 | Inhibition of 11beta-HSD1 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483810 | Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 50 mg/kg, po measured at 4 hrs by ELISA | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID657807 | Inhibition of mouse 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone as substrate by scintillation proximity assay | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483820 | Antiobesity activity in po dosed diet-induced obese mouse assessed as decrease in body weight administered via gavage BID for 13 days measured after day 13 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483793 | Bioavailability in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483781 | Displacement of [3H]-cortisone human 17beta-HSD1 expressed in Escherichia coli after 30 mins by scintillation proximity assay | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483798 | Clearance in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID657809 | Volume of distribution at steady state in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483783 | Inhibition of 11beta-HSD2 | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID1218575 | Clearance in iv dosed rat | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
| Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers. |
| AID483791 | Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID657814 | Volume of distribution at steady state in CD1 mouse at 2 mg/kg, iv and 10 mg/kg, po | 2011 | ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
| Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes. |
| AID483811 | Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 5 mg/kg, po measured at 8 hrs by ELISA | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483814 | Antidiabetic activity in diet-induced obese mouse assessed as decrease in fed blood glucose level at 25 to 50 mg/kg, po administered via gavage BID for 13 days measured after day 13 by glucose tolerance test | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483786 | Clearance in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID483809 | Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 15 mg/kg, po measured at 4 hrs by ELISA | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| AID1071799 | Inhibition of 11beta-HSD1 in human liver microsomes using cortisone as substrate after 2 hrs by HTRF assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
| 3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitor. |
| AID483796 | Terminal half life in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po | 2010 | Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
| Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |